About this Author

College chemistry, 1983

The 2002 Model

After 10 years of blogging. . .

Derek Lowe, an Arkansan by birth, got his BA from Hendrix College and his PhD in organic chemistry from Duke before spending time in Germany on a Humboldt Fellowship on his post-doc. He's worked for several major pharmaceutical companies since 1989 on drug discovery projects against schizophrenia, Alzheimer's, diabetes, osteoporosis and other diseases.
To contact Derek email him directly: derekb.lowe@gmail.com
Twitter: Dereklowe

October 14, 2010

Conference Thoughts

Posted by Derek

Update: here's a trip report on this conference over at Practical Fragments

I'm back from Philadelphia and the FBLD conference. I'm not going to put a trip report up on the blog - although I'm certainly writing one up for my colleagues at work - but a number of people at the meeting asked me what I might say about it here.

Well, I enjoyed it. I tend to like more focused conferences like this one, anyway, where most of the people doing the best work in a field can attend what's still a fairly small meeting. It probably helps that this isn't a very old series of meetings, too. Over time, some sort of scientific entropy sets in, and the topics covered can begin to smear out a bit. Some of the longer-running Gordon Conferences are (to me, anyway) a little blurry about what they're trying to cover.

That same tendency can affect individual talks. We medicinal chemists are particularly guilty of that, since our discipline spreads over a pretty wide area. At a meeting like this one, which was all about fragment-based techniques, people had to resist the temptation to keep going past the fragment-based parts of their talk. Once you get up toward 400 molecular weight, you're not talking about fragments any more - you're doing good old medicinal chemistry. Maybe it's structure-based at that point, maybe not, and maybe you're using some of the biophysical techniques that help out with moving fragment leads forward - but the fragment techniques are what got you to that point, not what's carrying you forward through the concerns about PK, formulations, polymorphs, and all the other later-stage worries of a drug program.

The speakers at this meeting generally did a good job avoiding this pitfall, but I have to admit that the few times I saw PK data come up on the screen, I stopped taking notes. I didn't stop listening, on the chance that there might be something interesting, but it certainly wasn't what I was there to focus on. One could imagine a whole meeting about solving PK problems in drug development - there probably is one, actually. But at that one, you'd have to make sure that the speakers didn't spend time telling you about the neat fragment-based techniques that led to their drug candidate.

As I said, though, there were a lot of interesting speakers at this one, and not a single talk was anything close to a complete waste of time. How many meetings can you say that about? Things ran smoothly, and with notably better food than some of the other conferences I've attended. Some meetings just pitch a bunch of Wissenschaftlerfutter out onto the tables, figuring that people will deal with it - and to be honest, they're usually right. We'll eat most anything in this field, although I've been told that physicists are even less discriminating, so at least we have that.

" but I have to admit that the few times I saw PK data come up on the screen, I stopped taking notes. I didn't stop listening, on the chance that there might be something interesting, but it certainly wasn't what I was there to focus on. One could imagine a whole meeting about solving PK problems in drug development - there probably is one, actually."

There is a whole profession, actually, it's called "clinical pharmacology". You may have heard of us...;^))

A quick thought on yesterdays post "A Cautionary Tale". With the amount of structural data available on cruzain it is a crime that these folks wasted any time at all on these compounds. It should have been obvious that these are not cruzain inhibitors. Especially since this was being done, in of all places, UCSF. A simple modeling experiment or qsar study would have told you that you were barking up the wrong tree. I am not a medicinal chemist but I try to play one in academia. If I were this student I would be very upset with my advisor for having wasted what looks to be a significant amount of my time on this. I keep hearing that the model for the future of big pharma will be that medicinal chemistry will be done in academic laboratories.....good luck trying to find a drug.